Details of the Target

General Information of Target

Target ID LDTP12756
Target Name ADP-ribosylhydrolase ARH3 (ADPRS)
Gene Name ADPRS
Gene ID 54936
Synonyms
ADPRHL2; ARH3; ADP-ribosylhydrolase ARH3; ADP-ribose glycohydrolase ARH3; ADP-ribosylhydrolase 3; O-acetyl-ADP-ribose deacetylase ARH3; EC 3.5.1.-; Poly(ADP-ribose) glycohydrolase ARH3; EC 3.2.1.143; [Protein ADP-ribosylarginine] hydrolase-like protein 2; [Protein ADP-ribosylserine] hydrolase; EC 3.2.2.-
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MNGRADFREPNAEVPRPIPHIGPDYIPTEEERRVFAECNDESFWFRSVPLAATSMLITQG
LISKGILSSHPKYGSIPKLILACIMGYFAGKLSYVKTCQEKFKKLENSPLGEALRSGQAR
RSSPPGHYYQKSKYDSSVSGQSSFVTSPAADNIEMLPHYEPIPFSSSMNESAPTGITDHI
VQGPDPNLEESPKRKNITYEELRNKNRESYEVSLTQKTDPSVRPMHERVPKKEVKVNKYG
DTWDE
Target Bioclass
Enzyme
Family
ADP-ribosylglycohydrolase family
Subcellular location
Nucleus
Function
ADP-ribosylhydrolase that preferentially hydrolyzes the scissile alpha-O-linkage attached to the anomeric C1'' position of ADP-ribose and acts on different substrates, such as proteins ADP-ribosylated on serine and threonine, free poly(ADP-ribose) and O-acetyl-ADP-D-ribose. Specifically acts as a serine mono-ADP-ribosylhydrolase by mediating the removal of mono-ADP-ribose attached to serine residues on proteins, thereby playing a key role in DNA damage response . Serine ADP-ribosylation of proteins constitutes the primary form of ADP-ribosylation of proteins in response to DNA damage. Does not hydrolyze ADP-ribosyl-arginine, -cysteine, -diphthamide, or -asparagine bonds. Also able to degrade protein free poly(ADP-ribose), which is synthesized in response to DNA damage: free poly(ADP-ribose) acts as a potent cell death signal and its degradation by ADPRHL2 protects cells from poly(ADP-ribose)-dependent cell death, a process named parthanatos. Also hydrolyzes free poly(ADP-ribose) in mitochondria. Specifically digests O-acetyl-ADP-D-ribose, a product of deacetylation reactions catalyzed by sirtuins. Specifically degrades 1''-O-acetyl-ADP-D-ribose isomer, rather than 2''-O-acetyl-ADP-D-ribose or 3''-O-acetyl-ADP-D-ribose isomers.
Uniprot ID
Q9NX46
Ensemble ID
ENST00000373178.5
HGNC ID
HGNC:21304
ChEMBL ID
CHEMBL4295963

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 10 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		13.42  LDD0402  [1]
STPyne
 Probe Info  		K131(8.46)  LDD0277  [2]
Probe 1
 Probe Info  		Y74(19.09); Y108(15.69); Y149(130.41)  LDD3495  [3]
DBIA
 Probe Info  		C132(0.97)  LDD3314  [4]
4-Iodoacetamidophenylacetylene
 Probe Info  		C287(0.00); C283(0.00)  LDD0038  [5]
IA-alkyne
 Probe Info  		C287(0.00); C132(0.00); C283(0.00)  LDD0036  [5]
Lodoacetamide azide
 Probe Info  		C287(0.00); C132(0.00); C283(0.00)  LDD0037  [5]
IPM
 Probe Info  		N.A.  LDD0025  [6]
NAIA_4
 Probe Info  		N.A.  LDD2226  [7]
NAIA_5
 Probe Info  		C132(0.00); C283(0.00)  LDD2223  [7]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HEK-293T C287(0.99)  LDD1507  [8]
 LDCM0237  AC12 HEK-293T C287(0.98)  LDD1510  [8]
 LDCM0259  AC14 HEK-293T C287(1.13)  LDD1512  [8]
 LDCM0270  AC15 HEK-293T C287(1.04)  LDD1513  [8]
 LDCM0276  AC17 HEK-293T C287(0.78)  LDD1515  [8]
 LDCM0280  AC20 HEK-293T C287(0.95)  LDD1519  [8]
 LDCM0281  AC21 HEK-293T C287(1.05)  LDD1520  [8]
 LDCM0282  AC22 HEK-293T C287(1.27)  LDD1521  [8]
 LDCM0283  AC23 HEK-293T C287(1.09)  LDD1522  [8]
 LDCM0285  AC25 HEK-293T C287(0.95)  LDD1524  [8]
 LDCM0288  AC28 HEK-293T C287(1.02)  LDD1527  [8]
 LDCM0289  AC29 HEK-293T C287(1.02)  LDD1528  [8]
 LDCM0291  AC30 HEK-293T C287(1.00)  LDD1530  [8]
 LDCM0292  AC31 HEK-293T C287(1.07)  LDD1531  [8]
 LDCM0294  AC33 HEK-293T C287(0.97)  LDD1533  [8]
 LDCM0297  AC36 HEK-293T C287(0.96)  LDD1536  [8]
 LDCM0298  AC37 HEK-293T C287(1.21)  LDD1537  [8]
 LDCM0299  AC38 HEK-293T C287(1.05)  LDD1538  [8]
 LDCM0300  AC39 HEK-293T C287(1.07)  LDD1539  [8]
 LDCM0301  AC4 HEK-293T C287(1.08)  LDD1540  [8]
 LDCM0303  AC41 HEK-293T C287(0.99)  LDD1542  [8]
 LDCM0306  AC44 HEK-293T C287(0.98)  LDD1545  [8]
 LDCM0307  AC45 HEK-293T C287(1.05)  LDD1546  [8]
 LDCM0308  AC46 HEK-293T C287(1.06)  LDD1547  [8]
 LDCM0309  AC47 HEK-293T C287(1.11)  LDD1548  [8]
 LDCM0311  AC49 HEK-293T C287(0.91)  LDD1550  [8]
 LDCM0312  AC5 HEK-293T C287(1.11)  LDD1551  [8]
 LDCM0315  AC52 HEK-293T C287(1.05)  LDD1554  [8]
 LDCM0316  AC53 HEK-293T C287(1.08)  LDD1555  [8]
 LDCM0317  AC54 HEK-293T C287(1.00)  LDD1556  [8]
 LDCM0318  AC55 HEK-293T C287(1.11)  LDD1557  [8]
 LDCM0320  AC57 HEK-293T C287(1.07)  LDD1559  [8]
 LDCM0323  AC6 HEK-293T C287(1.02)  LDD1562  [8]
 LDCM0324  AC60 HEK-293T C287(0.97)  LDD1563  [8]
 LDCM0325  AC61 HEK-293T C287(1.18)  LDD1564  [8]
 LDCM0326  AC62 HEK-293T C287(1.07)  LDD1565  [8]
 LDCM0327  AC63 HEK-293T C287(1.11)  LDD1566  [8]
 LDCM0334  AC7 HEK-293T C287(0.98)  LDD1568  [8]
 LDCM0248  AKOS034007472 HEK-293T C287(1.09)  LDD1511  [8]
 LDCM0356  AKOS034007680 HEK-293T C287(0.98)  LDD1570  [8]
 LDCM0156  Aniline NCI-H1299 11.89  LDD0403  [1]
 LDCM0632  CL-Sc Hep-G2 C132(0.18)  LDD2227  [7]
 LDCM0368  CL10 HEK-293T C287(1.23)  LDD1572  [8]
 LDCM0372  CL103 HEK-293T C287(1.11)  LDD1576  [8]
 LDCM0376  CL107 HEK-293T C287(1.07)  LDD1580  [8]
 LDCM0379  CL11 HEK-293T C287(1.09)  LDD1583  [8]
 LDCM0381  CL111 HEK-293T C287(1.19)  LDD1585  [8]
 LDCM0385  CL115 HEK-293T C287(1.00)  LDD1589  [8]
 LDCM0389  CL119 HEK-293T C287(0.95)  LDD1593  [8]
 LDCM0394  CL123 HEK-293T C287(1.10)  LDD1598  [8]
 LDCM0398  CL127 HEK-293T C287(0.99)  LDD1602  [8]
 LDCM0402  CL15 HEK-293T C287(0.94)  LDD1606  [8]
 LDCM0404  CL17 HEK-293T C287(0.85)  LDD1608  [8]
 LDCM0408  CL20 HEK-293T C287(1.16)  LDD1612  [8]
 LDCM0409  CL21 HEK-293T C287(1.10)  LDD1613  [8]
 LDCM0410  CL22 HEK-293T C287(1.21)  LDD1614  [8]
 LDCM0411  CL23 HEK-293T C287(0.98)  LDD1615  [8]
 LDCM0415  CL27 HEK-293T C287(1.13)  LDD1619  [8]
 LDCM0417  CL29 HEK-293T C287(0.91)  LDD1621  [8]
 LDCM0418  CL3 HEK-293T C287(0.89)  LDD1622  [8]
 LDCM0421  CL32 HEK-293T C287(0.91)  LDD1625  [8]
 LDCM0422  CL33 HEK-293T C287(1.00)  LDD1626  [8]
 LDCM0423  CL34 HEK-293T C287(1.11)  LDD1627  [8]
 LDCM0424  CL35 HEK-293T C287(1.01)  LDD1628  [8]
 LDCM0428  CL39 HEK-293T C287(1.00)  LDD1632  [8]
 LDCM0431  CL41 HEK-293T C287(0.97)  LDD1635  [8]
 LDCM0434  CL44 HEK-293T C287(1.09)  LDD1638  [8]
 LDCM0435  CL45 HEK-293T C287(1.22)  LDD1639  [8]
 LDCM0436  CL46 HEK-293T C287(1.28)  LDD1640  [8]
 LDCM0437  CL47 HEK-293T C287(1.21)  LDD1641  [8]
 LDCM0440  CL5 HEK-293T C287(1.15)  LDD1644  [8]
 LDCM0444  CL53 HEK-293T C287(0.99)  LDD1647  [8]
 LDCM0447  CL56 HEK-293T C287(0.96)  LDD1650  [8]
 LDCM0448  CL57 HEK-293T C287(0.90)  LDD1651  [8]
 LDCM0449  CL58 HEK-293T C287(1.33)  LDD1652  [8]
 LDCM0450  CL59 HEK-293T C287(0.92)  LDD1653  [8]
 LDCM0455  CL63 HEK-293T C287(1.15)  LDD1658  [8]
 LDCM0457  CL65 HEK-293T C287(0.97)  LDD1660  [8]
 LDCM0460  CL68 HEK-293T C287(1.23)  LDD1663  [8]
 LDCM0461  CL69 HEK-293T C287(1.02)  LDD1664  [8]
 LDCM0463  CL70 HEK-293T C287(1.16)  LDD1666  [8]
 LDCM0464  CL71 HEK-293T C287(0.97)  LDD1667  [8]
 LDCM0470  CL77 HEK-293T C287(0.94)  LDD1673  [8]
 LDCM0473  CL8 HEK-293T C287(0.95)  LDD1676  [8]
 LDCM0474  CL80 HEK-293T C287(1.12)  LDD1677  [8]
 LDCM0475  CL81 HEK-293T C287(1.00)  LDD1678  [8]
 LDCM0476  CL82 HEK-293T C287(1.16)  LDD1679  [8]
 LDCM0477  CL83 HEK-293T C287(1.10)  LDD1680  [8]
 LDCM0481  CL87 HEK-293T C287(1.20)  LDD1684  [8]
 LDCM0483  CL89 HEK-293T C287(0.97)  LDD1686  [8]
 LDCM0484  CL9 HEK-293T C287(0.98)  LDD1687  [8]
 LDCM0487  CL92 HEK-293T C287(0.97)  LDD1690  [8]
 LDCM0488  CL93 HEK-293T C287(1.08)  LDD1691  [8]
 LDCM0489  CL94 HEK-293T C287(1.15)  LDD1692  [8]
 LDCM0490  CL95 HEK-293T C287(1.25)  LDD1693  [8]
 LDCM0494  CL99 HEK-293T C287(1.17)  LDD1697  [8]
 LDCM0495  E2913 HEK-293T C287(0.87)  LDD1698  [8]
 LDCM0625  F8 Ramos C132(1.84)  LDD2187  [9]
 LDCM0572  Fragment10 Ramos C132(0.84)  LDD2189  [9]
 LDCM0573  Fragment11 Ramos C132(0.47)  LDD2190  [9]
 LDCM0574  Fragment12 Ramos C132(0.86)  LDD2191  [9]
 LDCM0575  Fragment13 Ramos C132(0.84)  LDD2192  [9]
 LDCM0576  Fragment14 Ramos C132(0.95)  LDD2193  [9]
 LDCM0579  Fragment20 Ramos C132(0.80)  LDD2194  [9]
 LDCM0580  Fragment21 Ramos C132(0.92)  LDD2195  [9]
 LDCM0582  Fragment23 Ramos C132(1.04)  LDD2196  [9]
 LDCM0578  Fragment27 Ramos C132(1.25)  LDD2197  [9]
 LDCM0586  Fragment28 Ramos C132(1.16)  LDD2198  [9]
 LDCM0588  Fragment30 Ramos C132(1.16)  LDD2199  [9]
 LDCM0589  Fragment31 Ramos C132(0.66)  LDD2200  [9]
 LDCM0590  Fragment32 Ramos C132(0.63)  LDD2201  [9]
 LDCM0468  Fragment33 HEK-293T C287(1.03)  LDD1671  [8]
 LDCM0596  Fragment38 Ramos C132(0.96)  LDD2203  [9]
 LDCM0566  Fragment4 Ramos C132(1.03)  LDD2184  [9]
 LDCM0610  Fragment52 Ramos C132(0.94)  LDD2204  [9]
 LDCM0614  Fragment56 Ramos C132(0.97)  LDD2205  [9]
 LDCM0569  Fragment7 Ramos C132(0.79)  LDD2186  [9]
 LDCM0571  Fragment9 Ramos C132(0.52)  LDD2188  [9]
 LDCM0022  KB02 Ramos C132(0.84)  LDD2182  [9]
 LDCM0023  KB03 Ramos C132(0.87)  LDD2183  [9]
 LDCM0024  KB05 IGR37 C132(0.97)  LDD3314  [4]
 LDCM0628  OTUB2-COV-1 HEK-293T C132(1.54)  LDD2207  [10]
 LDCM0131  RA190 MM1.R C132(1.41)  LDD0304  [11]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Poly [ADP-ribose] polymerase tankyrase-1 (TNKS) ARTD/PARP family O95271

References

1 Quantitative and Site-Specific Chemoproteomic Profiling of Targets of Acrolein. Chem Res Toxicol. 2019 Mar 18;32(3):467-473. doi: 10.1021/acs.chemrestox.8b00343. Epub 2019 Jan 15.
2 A Paal-Knorr agent for chemoproteomic profiling of targets of isoketals in cells. Chem Sci. 2021 Oct 15;12(43):14557-14563. doi: 10.1039/d1sc02230j. eCollection 2021 Nov 10.
Mass spectrometry data entry: PXD028270
3 An Azo Coupling-Based Chemoproteomic Approach to Systematically Profile the Tyrosine Reactivity in the Human Proteome. Anal Chem. 2021 Jul 27;93(29):10334-10342. doi: 10.1021/acs.analchem.1c01935. Epub 2021 Jul 12.
4 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
5 Enhancing Cysteine Chemoproteomic Coverage through Systematic Assessment of Click Chemistry Product Fragmentation. Anal Chem. 2022 Mar 8;94(9):3800-3810. doi: 10.1021/acs.analchem.1c04402. Epub 2022 Feb 23.
Mass spectrometry data entry: PXD028853
6 Chemoproteomic Profiling by Cysteine Fluoroalkylation Reveals Myrocin G as an Inhibitor of the Nonhomologous End Joining DNA Repair Pathway. J Am Chem Soc. 2021 Dec 8;143(48):20332-20342. doi: 10.1021/jacs.1c09724. Epub 2021 Nov 24.
Mass spectrometry data entry: PXD029255
7 N-Acryloylindole-alkyne (NAIA) enables imaging and profiling new ligandable cysteines and oxidized thiols by chemoproteomics. Nat Commun. 2023 Jun 15;14(1):3564. doi: 10.1038/s41467-023-39268-w.
Mass spectrometry data entry: PXD041264
8 Accelerating multiplexed profiling of protein-ligand interactions: High-throughput plate-based reactive cysteine profiling with minimal input. Cell Chem Biol. 2024 Mar 21;31(3):565-576.e4. doi: 10.1016/j.chembiol.2023.11.015. Epub 2023 Dec 19.
Mass spectrometry data entry: PXD044402
9 Site-specific quantitative cysteine profiling with data-independent acquisition-based mass spectrometry. Methods Enzymol. 2023;679:295-322. doi: 10.1016/bs.mie.2022.07.037. Epub 2022 Sep 7.
Mass spectrometry data entry: PXD027578
10 Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening. J Am Chem Soc. 2019 Jun 5;141(22):8951-8968. doi: 10.1021/jacs.9b02822. Epub 2019 May 22.
11 Physical and Functional Analysis of the Putative Rpn13 Inhibitor RA190. Cell Chem Biol. 2020 Nov 19;27(11):1371-1382.e6. doi: 10.1016/j.chembiol.2020.08.007. Epub 2020 Aug 27.